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Chromatin/Epigenetic PARP Rucaparib Camsylate

Rucaparib Camsylate

Catalog No. T16807   CAS 1859053-21-6

Rucaparib Camsylate is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.

Rucaparib Camsylate, CAS 1859053-21-6
Pack Size Availability Price/USD Quantity
2 mg In stock 52.00
5 mg In stock 74.00
10 mg In stock 131.00
25 mg In stock 228.00
50 mg In stock 358.00
100 mg In stock 638.00
200 mg In stock inquiry
500 mg In stock inquiry
1 mL * 10 mM (in DMSO) In stock 94.00
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Purity 99.80%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Rucaparib Camsylate is a PARP inhibitor (PARP1,Ki of 1.4 nM). Rucaparib Camsylate also displays binding affinity to eight other PARP domains.
Targets&IC50 PARP-1 : ic50 1.4 nM (ki)
In vivo Rucaparib is not toxic but obviously enhances temozolomide-induced TGD in the DNA repair protein-competent D384Med xenografts. Rucaparib and AG14584 obviously (P < 0.05) increase temozolomide toxicity. Rucaparib enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts. Rucaparib significantly potentiates the cytotoxicity of topotecan and temozolomide in NB-1691, SH-SY-5Y, and SKNBE (2c) cells. Rucaparib (1 mg/kg) significantly increases temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) results in a 50% increase in the temozolomide-induced tumor growth delay. Pharmacokinetics studies also show that Rucaparib is detected in the brain tissue, which indicates that Rucaparib has potential in intra-cranial malignancy therapy [1][3][4].
Molecular Weight 555.66
Formula C29H34FN3O5S
CAS No. 1859053-21-6

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 82.33 mg/mL(148.17 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956. 2. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264. 3. Daniel RA, et al. Central nervous system penetration and enhancement of temozolomide activity in childhood medulloblastoma models by poly(ADP-ribose) polymerase inhibitor AG-014699. Br J Cancer, 2010, 103(10), 1588-1596. 4. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.

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